Antimicrobials topical preparations

Boric acid is a weak bacteriostatic and antimicrobial agent, and has been used in topical preparations such as eye lotions. 

Phenylethyl alcohol is used as an antimicrobial preservative in nasal, ophthalmic, and otic formulations at 0.25-0.5% v/v concentration it is generally used in combination with other preservatives.Phenylethyl alcohol has also been used on its own as an antimicrobial preservative at concentrations up to 1% v/v in topical preparations. At this concentration, mycoplasmas are inactivated within 20 minutes, although enveloped viruses are resistant. " Phenylethyl alcohol is also used in flavors and as a perfumery component, especially in rose perfumes. 

Sodium sulfite is used as an antioxidant in applications similar to those for sodium metabisulfite It is also an effective antimicrobial preservative, particularly against fungi at low pH (0.1% w/v of sodium sulfite is used). Sodium sulfite is used in cosmetics, food products, and pharmaceutical applications such as parenteral formulations, inhalations, oral formulations, and topical preparations. 

Tea tree oil comes from an evergreen tree native to Australia. The herb has been used as a nonirritating, antimicrobial for cuts stings wounds burns and acne. It can be found in shampoos soaps and lotions. Tea tree oil should not be ingested orally but is effective when used topically for minor cuts and stings. Tea tree oil is used as an antifungal to relieve and control the symptoms of tinea pedis Topical application is most effective when used in a cream with at least 10% tea tree oil. Several commercially prepared ointments are available. The cream is applied to affected areas twice daily for several weeks... 

An example of a simple CZE method for peptide analysis and characterization is the one developed for protegrin IB-367.37 IB-367 is a peptide containing 17 amino acid residues that possess antimicrobial properties, and it is being developed for treatment of oral mucositis associated with aggressive cancer chemotherapy as well as other topical applications. This polycationic product was chemically synthesized using solid-phase and purified by preparative reversed-phase HPLC. IB-367 is rich in cysteine and arginine residues. 

About 120 chemical constituents have been identified in chamomile as secondary metabolites, including 28 terpenoids, 36 flavonoids and 52 additional compounds [4]. A substantial part of drag effects are determined by the essential oil content. Oil is collected from flower heads, either by steam distillation or solvent extraction, for yields of 0.24-1.90% of fresh or dry plant tissue. Among the essential oil constituents the most active are /-/-a-bisabolol and chamazulene. /-/-a-bisabolol has demonstrated anti-inflammatory, antispasmodic, antimicrobial, antiulcer, sedative and CNS activity. Chamazulene is also anti-inflammatory. Topical applications of chamomile preparation have shown benefit in the treatment of eczema, dermatitis and ulceration [5]. 

Rutala (1996) prepared a comprehensive set of guidelines for sporicidal agents to combat bacterial spores and in 1996 provided guidelines for the selection of topical and other antimicrobial agents. 

Gloor et al.82 discovered an additional antimicrobial activity of a distillate of Hamamelis (Aqua Hamamelidis) and urea formulated as a topical dermatological preparation that contains both active ingredients. Although mainly used for their antiinflammatory, hydrating, and barrier-stabilizing effects in dermatitis maintenance therapy, the antimicrobial activity of such products is considered a welcome, an added benefit. 

Topically administered ophthalmic preparations can affect visual acuity. Examples are lubricating gels and ointments for dry eye, antimicrobial ointments for ocular infections, and gel-forming solutions for glaucoma. Although acuity is only slightly reduced and is only temporary, this effect can be annoying to patients and may lead to noncompliance. 

Superficial bacterial infections, e.g. impetigo, eczema, are commonly staphylococcal or streptococcal. They are treated by a topical antimicrobial for less than 2 weeks and applied twice daily after removal of crusts that prevent access of the drug, e.g. by a povidone-iodine preparation. Very extensive cases need systemic treatment. 

The ototopical antimicrobial preparations stated earlier suffice for most cases of otitis externa and selected cases of chronic suppurative otitis. However, these compounds have a limited effect in certain patients with resistant strains of bacteria, drug-induced allergies, or a tympanic membrane perforation that requires administration into the middle ear space. In the last case, ototopical preparations may cause pain because of the acidic pH or the presence of alcohol. Ototoxicity of neomycin, polymyxin B, and colistin is also of concern, and many otolaryngologists prefer topical ophthalmic preparations.f Ophthalmic preparations are discussed in the article Ocular Drug Formulation and Delivery in this volume. 

Ciprofloxacin is well known for its wide range of bactericidal activity, especially against S. aureus. Staphylococcus epidermidis, and P. aeruginosa This preparation has the ideal antimicrobial spectrum for refractory otitis however topical therapy should not be considered alone for more serious infections such as those with underlying osteomyelitis. 

Ethanol and aqueous ethanol solutions of various concentrations (see Sections 8 and 17) are widely used in pharmaceutical formulations and cosmetics see Table 1. Although ethanol is primarily used as a solvent, it is also employed in solutions as an antimicrobial preservative. Topical ethanol solutions are also used as penetration enhancers " and as disinfectants. Ethanol has also been used in transdermal preparations in combination with Labrasol as a 7)... 

Benzethonium chloride is a quaternary ammonium compound used in pharmaceutical formulations as an antimicrobial preservative. Typically, it is used for this purpose in injections, ophthalmic and otic preparations at concentrations 0.01-0.02% w/v. Benzethonium chloride may also be used as a wetting and solubilizing agent, and as a topical disinfectant. 

Cresol is used at 0.15-0.3% concentration as an antimicrobial preservative in intramuscular, intradermal, and subcutaneous injectable pharmaceutical formulations. It is also used as a preservative in some topical formulations and as a disinfectant. Cresol is not suitable as a preservative for preparations that are to be freeze-dried. ... 

Methylparaben and other parabens are widely used as antimicrobial preservatives in cosmetics and oral and topical pharmaceutical formulations. Although parabens have also been used as preservatives in injections and ophthalmic preparations, they are now generally regarded as being unsuitable for these types of formulations owing to the irritant potential of the parabens. These experiences may depend on... 

Phenylmercuric salts are used as antimicrobial preservatives mainly in ophthalmic preparations, but are also used in cosmetics see Section 16), parenteral, and topical pharmaceutical formulations see Table I. 

Potassium sorbate is an antimicrobial preservative, with antibacterial and antifungal properties used in pharmaceuticals, foods, enteral preparations, and cosmetics. Generally, it is used at concentrations of 0.1-0.2% in oral and topical formulations, especially those containing nonionic surfactants. Potassium sorbate has been used to enhance the ocular bioavailability of timolol. 

Sodium metabisulfite is used as an antioxidant in oral, parenteral, and topical pharmaceutical formulations, at concentrations of 0.01-1.0% w/v. Primarily, sodium metabisulfite is used in acidic preparations for alkaline preparations, sodium sulfite is usually preferred see Section 18. Sodium metabisulfite also has some antimicrobial activity, which is greatest at acid pH, and may be used as a preservative in oral preparations such as syrups. 

Cinoiazepam [inn] is one of the [1,41 benzodiazepines, a BENZODIAZEPINE BINDING-SITE AGONIST, with most of its properties similar to diazepam. It has HYPNOTIC, ANTICONVULSANT and ANXIOLYTIC activity. It has been used orally to treat insomnia and anxiety, cinoxacin [ban, inn, jan, usan] (Clnobac ) is an ANTIMICROBIAL, One of a 4-quinolone family related to nalidixic acid, which, though symthetic, are sometimes described as ANTIBIOTICS. It can be used clinically as an ANTIBACTERIAL, mainly used orally for gut infections. Cinoxate [inn, usan] is a cinnamic acid derivative and can be used in topical sunscreen preparations. 

Treatments available for mouth ulcers are topical anti-inflammatories and preparations containing combinations of anaesthetic, analgesic, antimicrobial and astringent ingredients. 

Topical comedolytic, antibacterial and combined comedolytic/antimicrobial preparations. 

Isopropyl alcohol (2-propanol) is also commonly listed in the inactive ingredient guide for topical lotions (2.7 to 78%) and solutions (4 to 50%). Indeed, this alcohol is widely used at around 70% as an antimicrobial agent and has been shown to be effective for preoperative skin preparation (Keblish et al., 2005). However, isopropyl alcohol can also traverse human skin in significant amounts ten healthy adult volunteers applied a commercially available isopropyl alcohol-containing hand rub every 10 min over a 4 h period. Blood levels were recorded in 9 of the 10 volunteers at levels ranging from 0.5 tol.8 mg/1 (Turner et al., 2004). 

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